Takinib
Based on 33 publication(s) in Google Scholar
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
For research use only. We do not sell to patients.
- Purity : 99.68%
- CAS No.: 1111556-37-6
- Formula: C18H18N4O2
- Molecular Weight:322.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- Protocols
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) Takinib
More- Cancer Res. 2026 Jun 15.
- Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
- J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
- Cell Death Dis. 2024 Jun 21;15(6):438. [Abstract]
- ACS Cent Sci. 2018 Aug 22;4(8):982-995. [Abstract]
- Acta Pharmacol Sin. 2026 Mar 11. [Abstract]
- Cell Death Discov. 2025 Jul 25;11(1):345. [Abstract]
- Cell Chem Biol. 2026 Jun 18;33(6):767-784.e7. [Abstract]
- Int J Biol Macromol. 2026 Mar:349:150991. [Abstract]
- EMBO J. 2021 Nov 2;40(21):e108028. [Abstract]
- Antioxidants (Basel). 2021 Nov 26;10(12):1898. [Abstract]
- Clin Transl Med. 2022 Jun;12(6):e850. [Abstract]
- Cell Rep. 2024 Oct 8;43(10):114827. [Abstract]
- J Med Chem. 2025 Feb 13;68(3):2694-2719. [Abstract]
- J Ethnopharmacol. 2026 Jun 12:364:121516. [Abstract]
- Biochem Pharmacol. 2025 Mar:233:116764. [Abstract]
- Drug Des Devel Ther. 2025 Sep 30:19:8843-8864. [Abstract]
- J Cell Biol. 2018 Aug 6;217(8):2727-2742. [Abstract]
- J Am Heart Assoc. 2018 Dec 4;7(23):e03677. [Abstract]
- Eur J Pharmacol. 2023 May 15:947:175679. [Abstract]
- Int J Mol Sci. 2026 Apr 2;27(7):3232. [Abstract]
- Int Immunopharmacol. 2025 Jan 27:146:113842. [Abstract]
- Biogerontology. 2026 Jul 28;27(4):133.
- Am J Pathol. 2024 Dec;194(12):2290-2301. [Abstract]
- Mol Oncol. 2023 Nov;17(11):2356-2379. [Abstract]
- NPJ Syst Biol Appl. 2023 Nov 16;9(1):57. [Abstract]
- J Biol Chem. 2020 Oct 16;295(42):14325-14342. [Abstract]
- Mol Biol Cell. 2018 Oct 1;29(20):2470-2480. [Abstract]
- Biol Pharm Bull. 2020 Nov 1;43(11):1643-1652. [Abstract]
- bioRxiv. 2026 May 26:2026.05.24.727500. [Abstract]
- bioRxiv. 2025 Oct 1.
- Elife. 2022 Jun 28;11:e78044. [Abstract]
- J Pers Med. 2021 Sep 11;11(9):906. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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WB
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RT-PCR
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WB
All MAP3K Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
TAK1 9.5 nM (IC50) |
IRAK4 120 nM (IC50) |
IRAK1 390 nM (IC50) |
GCK 430 nM (IC50) |
CLK2 430 nM (IC50) |
MINK1 1.9 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MPC-11 | GI50 |
8.5 μM
Compound: Takinib
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Cytotoxicity against mouse MPC-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity against mouse MPC-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
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[PMID: 38283221] |
| NCI-H929 | GI50 |
51 μM
Compound: Takinib
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Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Blue assay
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[PMID: 38283221] |
In Vitro
Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1].
Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65[1].
Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria[3].
Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Breast cancer cell line MDA-MB-231
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Concentration:10 μM
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Incubation Time:5, 15, 30, 60 minutes
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Result:IKK and p65 were maximally phosphorylated at 15 minutes, which indicated activation of the NF-κB pathway, while p38 phosphorylation peaks at 30 minutes.
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Cell Line:IL-1β-treated (10 ng/mL; 30 min) RASFs
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Concentration:0.1-20 µM
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Incubation Time:2 hours
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Result:Induced phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727.
In Vivo
Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male DBA/1 mice (CIA arthritis model)[4]
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Dosage:50 mg/kg
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Administration:Intraperitoneally; daily from days 18-36
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Result:Showed a reduction in clinical arthritic score compared to vehicle control.
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Animal Model:Female NSG mice (8 weeks old)[5]
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Dosage:50 mg/kg
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Administration:Oral gavage; daily until 17 days
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Result:Slowed tumor growth and reduced tumor size/weight.
Chemical Information
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CAS No. 1111556-37-6
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Appearance Solid
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Molecular Weight 322.36
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Formula C18H18N4O2
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Color White to off-white
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SMILES
CCCN1C2=CC=CC=C2N=C1NC(C3=CC(C(N)=O)=CC=C3)=O
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Synonyms
EDHS-206
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (33)
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Journal Impact Factor
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Most Recent
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Nat Commun
Podocyte OTUD5 alleviates diabetic kidney disease through deubiquitinating TAK1 and reducing podocyte inflammation and injury. [Abstract]2024 Jun 27;15(1):5441. PMID: 38937512
Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
MPC5 cells transfected with si-OTUD5 were pretreated with 10 μM Takinib (TAK1 inhibitor) for 1 h before exposure to HG/PA. Levels of P-TAK1, P-ERK, P-P38, and P-JNK were detected by western blot.
Takinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 27;15(1):5441. [Abstract]
MPC5 cells transfected with si-OTUD5 were pretreated with 10 μM Takinib (TAK1 inhibitor) for 1 h before exposure to HG/PA. Real-time qPCR showing mRNA levels of Il6 and Tnfα.
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J Adv Res
Dual regulation of phaseol on osteoclast formation and osteoblast differentiation by targeting TAK1 kinase for osteoporosis treatment. [Abstract]2024 Dec 9:S2090-1232(24)00565-4. PMID: 39662728
Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
The activity of ALP in MCOBs following a 14-day exposure to OM with or without Takinib.
Takinib purchased from MedChemExpress. Usage Cited in: J Adv Res. 2024 Dec 9:S2090-1232(24)00565-4. [Abstract]
ARS staining of calcium deposition in MCOBs following a 21-day exposure to OM with or without Takinib (1 × magnification). Quantitative assessment of the calcium deposition.
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Cell Death Dis
Regulator of G protein signaling 16 restrains apoptosis in colorectal cancer through disrupting TRAF6-TAB2-TAK1-JNK/p38 MAPK signaling. [Abstract]2024 Jun 21;15(6):438. PMID: 38906869
Takinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 Jun 21;15(6):438. [Abstract]
The Caco-2 and SW480 cells were transfected with control and RGS16 siRNA for 48 h, and then treated with DMSO or Takinib for 8 h. The RGS16 and the activation of indicated protein were examined by Western blotting.
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ACS Cent Sci
Immunomodulation of the NLRP3 Inflammasome through Structure-Based Activator Design and Functional Regulation via Lysosomal Rupture. [Abstract]2018 Aug 22;4(8):982-995. PMID: 30159395 -
Acta Pharmacol Sin
2026 Mar 11. PMID: 41813972 -
Cell Death Discov
RIPK1 S213E mutant suppresses RIPK1-dependent cell death by preventing interactions with RIPK3 and CASP8. [Abstract]2025 Jul 25;11(1):345. PMID: 40715038 -
Cell Chem Biol
The cytotoxic effect of prexasertib is a consequence of dual inhibition on both CHK1 and AMPK. [Abstract]2026 Jun 18;33(6):767-784.e7. PMID: 42061410 -
Int J Biol Macromol
Rabies virus matrix protein hijacks the TGF-beta activated kinase 1 binding protein 2-p38 mitogen-activated protein kinase pathway to inhibit apoptosis and promote viral replication. [Abstract]2026 Mar:349:150991. PMID: 41713525 -
EMBO J
2021 Nov 2;40(21):e108028. PMID: 34472622 -
Antioxidants (Basel)
2021 Nov 26;10(12):1898. PMID: 34942999 -
Clin Transl Med
Uterus globulin associated protein 1 (UGRP1) binds podoplanin (PDPN) to promote a novel inflammation pathway during Streptococcus pneumoniae infection. [Abstract]2022 Jun;12(6):e850. PMID: 35652821 -
Cell Rep
Polo-like kinase 2 promotes microglial activation via regulation of the HSP90α/IKKβ pathway. [Abstract]2024 Oct 8;43(10):114827. PMID: 39383034 -
J Med Chem
Design and Synthesis of Hederagenin Derivatives for the Treatment of Sepsis by Targeting TAK1 and Regulating the TAK1-NF-κB/MAPK Signaling. [Abstract]2025 Feb 13;68(3):2694-2719. PMID: 39817810 -
J Ethnopharmacol
Nephropathy 1 Formula (N1F) mitigates cisplatin-induced acute kidney injury by inhibiting TAK1-dependent NF-κB signaling. [Abstract]2026 Jun 12:364:121516. PMID: 41812937 -
Biochem Pharmacol
Downregulation of RSAD2 ameliorates keratinocyte hyperproliferation and skin inflammation in psoriasis via the TAK1/NF-κB axis. [Abstract]2025 Mar:233:116764. PMID: 39848474 -
Drug Des Devel Ther
Emodin Alleviates Monocrotaline-Induced Pulmonary Arterial Hypertension by Directly Targeting TAK1. [Abstract]2025 Sep 30:19:8843-8864. PMID: 41049040 -
J Cell Biol
Endosomal TLR3, TLR7, and TLR8 control neuronal morphology through different transcriptional programs. [Abstract]2018 Aug 6;217(8):2727-2742. PMID: 29777026 -
J Am Heart Assoc
2018 Dec 4;7(23):e03677. PMID: 30571597 -
Eur J Pharmacol
RIP2 inhibition alleviates lipopolysaccharide-induced septic cardiomyopathy via regulating TAK1 signaling. [Abstract]2023 May 15:947:175679. PMID: 36967078 -
Int J Mol Sci
2026 Apr 2;27(7):3232. PMID: 41977413 -
Int Immunopharmacol
Astragaloside IV ameliorates atherosclerosis by targeting TAK1 to suppress endothelial cell proinflammatory activation. [Abstract]2025 Jan 27:146:113842. PMID: 39706043 -
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Am J Pathol
Lipopolysaccharide Triggers Luminal Acidification to Promote Defense Against Bacterial Infection in Vaginal Epithelium. [Abstract]2024 Dec;194(12):2290-2301. PMID: 39222908 -
Mol Oncol
Proximity proteomics reveals role of Abelson interactor 1 in the regulation of TAK1/RIPK1 signaling. [Abstract]2023 Nov;17(11):2356-2379. PMID: 36635880 -
NPJ Syst Biol Appl
Modulating the dynamics of NFκB and PI3K enhances the ensemble-level TNFR1 signaling mediated apoptotic response. [Abstract]2023 Nov 16;9(1):57. PMID: 37973854 -
J Biol Chem
2020 Oct 16;295(42):14325-14342. PMID: 32796029 -
Mol Biol Cell
2018 Oct 1;29(20):2470-2480. PMID: 30091641
Takinib purchased from MedChemExpress. Usage Cited in: Mol Biol Cell. 2018 Oct 1;29(20):2470-2480. [Abstract]
WT and WDR62-KO cells are pre-incubated withTakinib (2 µM) for 1 h then treated with TNFα (50 ng/mL) for 15 min. JNK activation is determined by Western blotting.
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Biol Pharm Bull
Sinomenine Inhibited Interleukin-1β-Induced Matrix Metalloproteinases Levels via SOCS3 Up-Regulation in SW1353 Cells. [Abstract]2020 Nov 1;43(11):1643-1652. PMID: 32879146 -
bioRxiv
2026 May 26:2026.05.24.727500. PMID: 42244601 -
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Elife
Domain fusion TLR2-4 enhances the autophagy-dependent clearance of Staphylococcus aureus in the genetic engineering goat. [Abstract]2022 Jun 28;11:e78044. PMID: 35762728 -
J Pers Med
GPR30 Activation by 17β-Estradiol Promotes p62 Phosphorylation and Increases Estrogen Receptor α Protein Expression by Inducing Its Release from a Complex Formed with KEAP1. [Abstract]2021 Sep 11;11(9):906. PMID: 34575683
Solvent & Solubility
In Vitro:
DMSO : 2.5 mg/mL (7.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (292 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039. [Content Brief]
[2]. Scarneo SA, et.al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res Ther. 2019 Dec 17;21(1):292. [Content Brief]
[3]. Raphemot R, et al. Plasmodium PK9 Inhibitors Promote Growth of Liver-Stage Parasites. Cell Chem Biol. 2019 Mar 21;26(3):411-419.e7. [Content Brief]
[4]. Panipinto PM, et.al. Takinib Inhibits Inflammation in Human Rheumatoid Arthritis Synovial Fibroblasts by Targeting the Janus Kinase-Signal Transducer and Activator of Transcription 3 (JAK/STAT3) Pathway. Int J Mol Sci. 2021;22(22):12580. Published 2021 Nov 22. [Content Brief]
[5]. Song Z,et.al. Essential role of the linear ubiquitin chain assembly complex and TAK1 kinase in A20 mutant Hodgkin lymphoma. Proc Natl Acad Sci U S A. 2020 Nov 17;117(46):28980-28991. [Content Brief]
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1021 mL | 15.5106 mL | 31.0212 mL | 77.5530 mL |
| 5 mM | 0.6204 mL | 3.1021 mL | 6.2042 mL | 15.5106 mL |
Takinib Related Classifications
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